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| 25mg |
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Purity: ≥98%
RRx-001 (RRx001; ABDNAZ) is a novel hypoxia-selective epigenetic modulator with potential radiosensitizing and anticancer activity. It binds to hemoglobin, inhibits glucose 6-phosphate dehydrogenase (G6PD) in human tumor cells, and promotes RBC-mediated redox reactions in hypoxic conditions. A novel, non-toxic epigenetic anticancer drug for a variety of tumor types, RRx-001 works by increasing the production of nitric oxide (NO) and inhibiting PPP. In several cell lines and tumor models, the novel, nonexplosive molecule RRx-001, which was derived from a class of solid rocket propellants, has shown promise as a novel cancer therapeutic agent.
| Targets |
G6PD; Nrf2-ARE
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| ln Vitro |
Glucose 6 phosphate dehydrogenase (G6PD), a crucial enzyme in the pentose phosphate pathway, is in charge of ensuring that adequate levels of the main cellular reductant, NADPH, are kept in the body. This is how RRx-001 exerts its anti-proliferative effect, at least in part. In three distinct cancer cell lines, Hep G2, CACO-2, and HT-29, RRx-001 alters the activity of the glucose and G6PD enzymes. The concentration-dependent effects of RRx-001 resulted in G6PD inhibition and increased glucose consumption. By producing ROS/RNS, RRx-001 activates p53 and PARP-1. It exerts anticancer activity, at least in part, by interfering with 3 crucial metabolic demands of rapidly proliferating cells: bioenergetics, macromolecular biosynthesis, and control of cytosolic redox homeostasis in living cells[1]. HO-1 and NQO1—two of Nrf2's downstream enzymes—are activated and translocated to the nucleus in tumor cells as a result of RRx-001. Other than epigenetic changes, RRx-001 works through pleiotropic mechanisms that involve redox signaling and redox-induced dysregulation of numerous signal pathways, including Nrf2, p53, PARP cleavage, HIF1 alpha, and G6PD activity. Along with deregulating cancer cell energetics and metabolism, it also activates p53 and p21 in response to double-stranded DNA breaks. By producing ROS and RNS, the drug RRx-001 effectively activates the Nrf2-ARE signaling pathway[3].
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| ln Vivo |
RRx-001 shows promise for short-term blood flow redistribution in tumors with a pericyte- and α-SMA-rich vasculature[2]. RRx-001 monotherapy is well tolerated and free of toxicities that would limit its dosage. It not only helps Nrf2 move into the nucleus, but it also increases endogenous Nrf2 expression in mouse SCC VII tumors[3].
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| Cell Assay |
Cell growth and proliferation is assessed using the MTT proliferation assay kit. In a nutshell, 96-well plates with 5×103 cells in each well are used to treat or leave untreated cells. Up to 72 hours can pass during cell culture. Each well is given 10 μL of MTT reagent before being left to sit for 3 hours. Following incubation, the culture medium is taken out, 100 μL of Crystal Dissolving Solution is poured into each well, and the solution's absorbance at 570 nm is gauged. In triplicate, MTT assays are carried out on samples from the same conditions. Adding MTT solution (0.5 mg/mL), allowing cells to incubate for 4 hours at 37 degrees Celsius, and then measuring absorption at 540 nm with a microplate reader are the steps in short order.
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| References |
| Molecular Formula |
C5H6BRN3O5
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| Molecular Weight |
268.02
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| Exact Mass |
266.9491
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| Elemental Analysis |
C, 22.41; H, 2.26; Br, 29.81; N, 15.68; O, 29.85
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| CAS # |
925206-65-1
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
C1C(CN1C(=O)CBr)([N+](=O)[O-])[N+](=O)[O-]
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| InChi Key |
JODKFOVZURLVTG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C5H6BrN3O5/c6-1-4(10)7-2-5(3-7,8(11)12)9(13)14/h1-3H2
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| Chemical Name |
2-bromo-1-(3,3-dinitroazetidin-1-yl)ethanone
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.33 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.33 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.33 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7311 mL | 18.6553 mL | 37.3106 mL | |
| 5 mM | 0.7462 mL | 3.7311 mL | 7.4621 mL | |
| 10 mM | 0.3731 mL | 1.8655 mL | 3.7311 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05566041 | Active Recruiting |
Drug: RRx-001 + eLOOP Device |
Carcinoma, Small Cell Lung | EpicentRx, Inc. | August 1, 2022 | Phase 3 |
| NCT02518958 | Completed | Drug: RRx-001 Drug: Nivolumab |
Lymphoma Malignant Solid Tumor |
EpicentRx, Inc. | July 21, 2015 | Phase 1 |
| NCT02096354 | Completed | Drug: RRx-001 Drug: Regorafenib Drug: Irinotecan |
Colorectal Neoplasms | EpicentRx, Inc. | May 2014 | Phase 2 |
| NCT03515538 | Completed | Drug: Cisplatin for injection | Oral Mucositis | EpicentRx, Inc. | July 12, 2018 | Phase 2 |
| NCT01359982 | Completed | Drug: RRx-001 | Lymphomas Malignant Solid Tumor |
EpicentRx, Inc. | September 2011 | Phase 1 |
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